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PE20040767A1 - Derivado hemisulfato de azido citosina cristalino anhidro - Google Patents

Derivado hemisulfato de azido citosina cristalino anhidro

Info

Publication number
PE20040767A1
PE20040767A1 PE2003001233A PE2003001233A PE20040767A1 PE 20040767 A1 PE20040767 A1 PE 20040767A1 PE 2003001233 A PE2003001233 A PE 2003001233A PE 2003001233 A PE2003001233 A PE 2003001233A PE 20040767 A1 PE20040767 A1 PE 20040767A1
Authority
PE
Peru
Prior art keywords
refers
hemisulphate
anhydro
crystalline
derivative
Prior art date
Application number
PE2003001233A
Other languages
English (en)
Inventor
Joseph Armstrong Martin
Anthony Prince
Keshab Sarma
Terrence Joseph Connolly
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20040767A1 publication Critical patent/PE20040767A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

SE REFIERE A LA SAL HEMISULFATO DE 1-[4(S)-AZIDO-2(S),3(R)-DIHIDROXI-4-(HIDROXIMETIL)-1(R)-CICLOPENTIL]CITOSINA DE FORMULA (Ia) QUE PRESENTA UNA MAYOR ESTABILIDAD Y MEJORES PROPIEDADES FISICAS, DICHA SAL DE HEMISULFATO PRESENTA 3 FORMAS CRISTALINAS POLIMORFICAS. LA FORMA A CON UNA HUELLA DE DIFRACCION DE POLVO POR RAYOS X ,TIENEN UNA DISTANCIAS D CON UN RANGO DE 17.5556 A 2.9787, LA FORMA B TIENE UN RANGO DE 2.8037 A 2.6227 Y LA FORMA C DE 7.7865 A 2.7752. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION DE ESTAS SALES, QUE COMPRENDE LA CRISTALIZACION DEL COMPUESTO A PARTIR DE UNA SOLUCION ENVEJECIDA DE ACIDO SULFURICO EN ETANOL PARA LA FORMA A, UNA SOLUCION DE ISOPROPANOL/AGUA (85:15) PARA LA FORMA B Y (60:40) PARA LA FORMA C, AMBAS EN PRESENCIA DE ACIDO SULFURICO. ADEMAS SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE LO CONTIENE Y A UN METODO PARA EL TRATAMIENTO DE UNA ENFERMEDAD INDUCIDA POR EL VIRUS DE LA HEPATITIS C
PE2003001233A 2002-12-09 2003-12-05 Derivado hemisulfato de azido citosina cristalino anhidro PE20040767A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US43188502P 2002-12-09 2002-12-09

Publications (1)

Publication Number Publication Date
PE20040767A1 true PE20040767A1 (es) 2004-11-06

Family

ID=32507815

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003001233A PE20040767A1 (es) 2002-12-09 2003-12-05 Derivado hemisulfato de azido citosina cristalino anhidro

Country Status (32)

Country Link
US (1) US6864244B2 (es)
EP (1) EP1572711B1 (es)
JP (1) JP4563818B2 (es)
KR (1) KR100675544B1 (es)
CN (1) CN1314697C (es)
AR (1) AR042312A1 (es)
AT (1) ATE430755T1 (es)
AU (1) AU2003292212B2 (es)
BR (1) BR0317146A (es)
CA (1) CA2506532C (es)
CY (1) CY1109296T1 (es)
DE (1) DE60327554D1 (es)
DK (1) DK1572711T3 (es)
ES (1) ES2324654T3 (es)
GT (1) GT200300276A (es)
HR (1) HRP20050503A2 (es)
IL (1) IL168685A (es)
JO (1) JO2542B1 (es)
MX (1) MXPA05006044A (es)
MY (1) MY130927A (es)
NO (1) NO330454B1 (es)
NZ (1) NZ540297A (es)
PA (1) PA8590701A1 (es)
PE (1) PE20040767A1 (es)
PL (1) PL213734B1 (es)
PT (1) PT1572711E (es)
RU (1) RU2334756C2 (es)
SI (1) SI1572711T1 (es)
TW (1) TWI294882B (es)
UY (1) UY28109A1 (es)
WO (1) WO2004052906A1 (es)
ZA (1) ZA200504472B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001017968A1 (en) * 1999-09-02 2001-03-15 Shionogi & Co., Ltd. Integrase inhibitors containing aromatic heterocycle derivatives
CA2284459C (en) 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
US20050182252A1 (en) * 2004-02-13 2005-08-18 Reddy K. R. Novel 2'-C-methyl nucleoside derivatives
CN101044151B (zh) * 2004-08-23 2011-01-19 弗·哈夫曼-拉罗切有限公司 抗病毒的4'-叠氮基-核苷
EA018935B1 (ru) * 2006-10-10 2013-11-29 Медивир Аб Нуклеозидный ингибитор для вгс (hcv)
AU2007342367B2 (en) 2007-01-05 2012-12-06 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
GB0709791D0 (en) * 2007-05-22 2007-06-27 Angeletti P Ist Richerche Bio Antiviral agents
GB0900914D0 (en) 2009-01-20 2009-03-04 Angeletti P Ist Richerche Bio Antiviral agents
AU2011305652B2 (en) 2010-09-22 2016-10-20 Janssen Biopharma, Inc. Azido nucleosides and nucleotide analogs
AU2015217221A1 (en) 2014-02-13 2016-08-11 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
CN103965116B (zh) * 2014-05-06 2016-06-15 中国科学院苏州纳米技术与纳米仿生研究所 半5-氟胞嘧啶盐、其制备方法及应用
CN106687118A (zh) 2014-07-02 2017-05-17 配体药物公司 前药化合物及其用途
US9828410B2 (en) 2015-03-06 2017-11-28 Atea Pharmaceuticals, Inc. β-D-2′-deoxy-2′-α-fluoro-2′-β-C-substituted-2-modified-N6-substituted purine nucleotides for HCV treatment
EP4088725A1 (en) 2016-09-07 2022-11-16 ATEA Pharmaceuticals, Inc. 2'-substituted-n6-substituted purine nucleotides for the treatment of a virus from the picornaviridae family
HRP20250266T1 (hr) 2017-02-01 2025-04-25 Atea Pharmaceuticals, Inc. Nukleotid hemi-sulfat sol za liječenje virusa hepatitisa c
JP2021509907A (ja) 2018-01-09 2021-04-08 リガンド・ファーマシューティカルズ・インコーポレイテッド アセタール化合物およびその治療的使用
JP2021521118A (ja) 2018-04-10 2021-08-26 アテア ファーマシューティカルズ, インコーポレイテッド 肝硬変を伴うhcv感染患者の治療
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
EP4355319A4 (en) 2021-06-17 2025-01-22 ATEA Pharmaceuticals, Inc. BENEFICIAL ANTI-HCV COMBINATION THERAPY
CN115536710B (zh) * 2022-10-18 2024-04-16 南京工业大学 一种高品质胞苷硫酸盐晶体的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5449664A (en) * 1988-11-21 1995-09-12 Syntex (U.S.A.) Inc. Antiviral agents
NO171507C (no) * 1988-11-21 1993-03-24 Syntex Inc Analogifremgangsmaate ved fremstilling av terapeutisk aktive nukleotidderivater
AU7623991A (en) * 1990-05-17 1991-11-21 Syntex (U.S.A.) Inc. Antiviral agents
ATE238328T1 (de) * 1996-10-16 2003-05-15 Ribapharm Inc Monozyklische l-nukleoside, analoga und ihre anwendungen
US20030008841A1 (en) * 2000-08-30 2003-01-09 Rene Devos Anti-HCV nucleoside derivatives
EP1539188B1 (en) * 2001-01-22 2015-01-07 Merck Sharp & Dohme Corp. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
GB0114286D0 (en) * 2001-06-12 2001-08-01 Hoffmann La Roche Nucleoside Derivatives

Also Published As

Publication number Publication date
HK1085483A1 (en) 2006-08-25
EP1572711A1 (en) 2005-09-14
EP1572711B1 (en) 2009-05-06
AU2003292212B2 (en) 2009-10-01
SI1572711T1 (sl) 2009-08-31
ES2324654T3 (es) 2009-08-12
WO2004052906A1 (en) 2004-06-24
TWI294882B (en) 2008-03-21
NO20052732D0 (no) 2005-06-07
HRP20050503A2 (en) 2006-12-31
CN1723215A (zh) 2006-01-18
ATE430755T1 (de) 2009-05-15
UY28109A1 (es) 2004-06-30
RU2334756C2 (ru) 2008-09-27
NZ540297A (en) 2007-05-31
IL168685A (en) 2010-11-30
NO330454B1 (no) 2011-04-18
PL377472A1 (pl) 2006-02-06
NO20052732L (no) 2005-09-06
CA2506532C (en) 2011-09-20
MXPA05006044A (es) 2005-08-18
PT1572711E (pt) 2009-06-25
PL213734B1 (pl) 2013-04-30
JP2006510649A (ja) 2006-03-30
KR20050084217A (ko) 2005-08-26
PA8590701A1 (es) 2004-11-26
US20040162265A1 (en) 2004-08-19
AU2003292212A1 (en) 2004-06-30
DE60327554D1 (de) 2009-06-18
ZA200504472B (en) 2006-02-22
JO2542B1 (en) 2010-09-05
DK1572711T3 (da) 2009-07-13
CA2506532A1 (en) 2004-06-24
CY1109296T1 (el) 2014-07-02
CN1314697C (zh) 2007-05-09
GT200300276A (es) 2004-09-02
BR0317146A (pt) 2005-10-25
US6864244B2 (en) 2005-03-08
MY130927A (en) 2007-07-31
AR042312A1 (es) 2005-06-15
TW200502243A (en) 2005-01-16
JP4563818B2 (ja) 2010-10-13
KR100675544B1 (ko) 2007-01-30
RU2005121927A (ru) 2006-01-27

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